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Published on March 8, 2014

Author: Hakanolak1


DENTIFRICES AND MOUTHWASHES INGREDIENTS AND THEIR USE Dr. Hakan ÇOLAK DDS, PhD Ishık University School of Dentistry Department of Conservative Dentistry

HISTORY • People of all times have been interested in their dental health, and toothpastes have ancient roots. • There is found a prescription of a toothpaste that can be dated back to the time b.c. in Ebers Papyrus, an Egyptian medical reference book.

HISTORY • Hippocrates (460-377 b.c.) – generally considered to be the first to recommend the use of a dentifrice


Toothpastes • Toothpastes – A toothpaste in defined as a semi-aqueous material for removing naturally occurring deposits from teeth and is supposed to be used simultaneous with a toothbrush. The main components of toothpastes are given in Table 1

Mouthwashes • A mouthwash is defined as a non-sterile aqueous solution used mostly for its deodorant, refreshing or antiseptic effect. • Mouthwashes or rinses are designed to reduce oral bacteria, remove food particles, temporary reduce bad breathe and provide a pleasant taste

Mouthwashes • Mouth rinses are generally classified as either cosmetic or therapeutic or a combination of the two.

Mouthwashes • Cosmetic rinses – commercial over-the-counter products that • • • • help remove oral debris before or after brushing, temporary suppress bad breath, diminish bacteria in the mouth refresh the mouth with a pleasant taste.

Mouthwashes • Therapeutic rinses – often have the benefits of their cosmetic counterparts, – but also contain an added active ingredient, f. ex. fluoride or chlorhexidine, that help protect against some oral diseases

Mouthwashes • The amount of the different components in mouthwashes varies from product to product. • Some practically have the same composition as toothpastes, although they do not contain abrasives. • Distinct from toothpastes most mouth rinses contain alcohol, as a preservative and a semiactive ingredient . • The amount of alcohol is usually ranging from 18 – 26 %


ABRASIVES • An abrasive is a substance that is used for abrading, grinding or polishing . • The degree of abrasivity depends on the; – hardness of the abrasive, – the morphology of the particles, – the concentration of abrasive in the paste. • The abrasives found in toothpastes are often not as hard as the enamel, but as hard or harder than the dentine

ABRASIVES • Most often found as crystals, small and smooth particles are preferred to avoid tooth wear. • Transparent toothpastes, – commonly called gel toothpastes, – are obtained by mixing certain abrasives. • The amount and type of abrasive in toothpaste – contributes to give the toothpaste its creamy consistency. • The abrasive effect is measured in the RDA (Radioactive Dentine Abrasion) scale, ranging from 40-80 in most toothpaste. • Hydrated silica – is a common abrasive in dentifrices; – alumina and calcium carbonate may also be used

THICKENING/BINDING AGENTS • prevent the toothpaste from drying out by binding water. • control the viscosity and contribute to give the toothpaste a creamy consistency. • have an emulsifying effect by preventing the solid and the liquid substances from separating and give the possibility to make oil in water emulsions.

THICKENING/BINDING AGENTS • Common water-binding substances – Glycerol, – Sorbitol, – Polyethylene glycol (PEG), – Propylene glycol – Cellulose Gum • Thickening agents • Carageenan • Carbomer

HUMECTANTS • Short-chained polyalcohols • used in toothpastes to prevent loss of water, and subsequent hardening of the paste, when it is exposed to air. • They also provide creamy texture. • Glycerine and sorbitol are frequently used.

SOLVENTS • Water is the most common solvent used in toothpaste. It dissolves the ingredients and allows them to be mixed. • Alcohol is used in mouth rinses as a solvent and taste enhancer.

DETERGENTS (SURFACTANTS) • Detergents are cleansing or purging agents that through a surface action that depends on their possessing both hydrophilic and hydrophobic properties, exerts cleansing (oil-dissolving) and antibacterial effects

DETERGENTS (SURFACTANTS) • Detergents lower the surface tension of the liquid environment in the oral cavity – the substances in the toothpaste/mouthwash can contact the teeth more easily. • They penetrate and dissolve plaque. – This makes it easies to clean the teeth. • The foaming effect – beneficial in cleaning the teeth – contributes to remove debris and gives a feeling of cleanness. • Helping dispersing the flavours in the toothpaste/mouthwash.

DETERGENTS (SURFACTANTS) • Sodium Lauryl Sulphate (SLS) – the most widely used detergent • SLS may have some adverse effects including – damaging the mucin layer by denaturizing its glycoprotein – an increased frequency of recurrent aphthous – ulcers (RAU) in some patients

FLAVOURING AGENTS • Generally combinations of water-insoluble essential oils are used – spearmint, – peppermint, – eucalyptus and – menthol

FLAVOURING AGENTS • Toothpastes and mouthwashes often have a very strong flavour. – This is necessary to cover the horrid taste of most detergents, especially SLS. • Flavouring agents are also added to meet the customers demand for a fresh sensation during and after brushing the teeth or rinsing the mouth • Usually the flavouring agents represent the main cost of the raw materials, approximately 60 %.

SWEETENERS • improve the taste of toothpastes and mouthwashes and give them a mild and sweet taste. • The most common used sweeteners are – sodium saccharin, – sorbitol – glycerin – xylitol

COLOURING AGENTS • Most toothpastes and mouthwashes contain colour-substances to give them an attractive appearance. • The colour-substances are classified by the Colour Index (CI), published by the Society of Dyers and Colourists and the American Association of Textile Chemists and Colourists, or by a system called the F D & C Colours • Titanium dioxide is often added to toothpastes to give them a white, opaque colour.

PRESERVATIVES • prevent the growth of micro-organisms in toothpastes and mouthwashes. • Common preservatives include – sodium benzoate, – methylparaben – ethylparaben.

ANTI-CARIES AGENTS • Fluoride: – considered to be the most effective caries-inhibiting agent, and almost all toothpastes today contain fluoride in one form or the other – The most common form is sodium fluoride (NaF), but mono-fluoro-phosphate (MFP) and stannous fluoride (SnF) are also used – Fluoride is most beneficial when the mouth is not rinsed with water after tooth brushing. In this way a bigger amount of fluoride is retained in the oral cavity

Fluoride: • There are three main theories considering the positive action of fluoride in the prevention of caries:

positive action of fluoride in the prevention of caries: • It is claimed that fluoride, incorporated into the enamel during tooth development in the form of fluorhydroxyapatite (FAP), reduces the solubility of the apatite. • This theory implies that “caries resistance”, once obtained, will last always.

positive action of fluoride in the prevention of caries: • anti-bacterial actions – In an acidic environment, if fluoride is present, hydrogen fluoride (HF) is formed. – HF is an undissociated, week acid that can penetrate the bacterial cell membrane. The entry of HF into the alkaline cytoplasmic compartments results in dissociation of HF to H+ and F

positive action of fluoride in the prevention of caries: • the most important anti-caries effect is claimed to be due to the formation of calcium fluoride (CaF2) in plaque and on the enamel surface during and after rinsing or brushing with fluoride.

positive action of fluoride in the prevention of caries: • CaF2 serves as a fluoride reservoir. • When the pH drops, fluoride and calcium are released into the plaque fluid. • Fluoride diffuses with the acid from plaque into the enamel pores and forms fluoroapatite (FAP). • FAP incorporated in the enamel surface is more resistant to a subsequent acid attack since the critical pH of FAP (pH=4.5) is lower than that of hydroxyapatite (HA) (pH=5.5).

Xylitol • Sugar alcohol • cannot be fermentated by oral microorganisms. • It is considered to be a cariostatic agent since it can inhibit the carbohydrate metabolism in different oral micro-organisms • unique among the sugar alcohols in its inhibitory effect on glycolysis.

Sodium Bicarbonate • Several studies have shown that bicarbonate is one of the salivary components that potentially modifies the formation of caries. • It increases the pH in saliva, and in this way creates a hostile environment for the growth of aciduric bacteria.

ANTI-PLAQUE AGENTS • Sodium Lauryl Sulphate (SLS): – It has been shown that the enzymes glucosyltransferase and fructosyltransferase are incorporated in an active form into the pellicle; and by synthesizing glucan in situfrom sucrose, can provide a surface for colonization by Streptococcus mutans. – These enzymes can be inhibited by SLS. Such inhibition can clearly retard the regrowth of plaque

ANTI-PLAQUE AGENTS • Triclosan: – synthetic non-ionic chlorinated phenolic agent with antiseptic qualities – has a broad-spectrum efficacy on Gram-positive and most Gram-negative bacteria.tic qualities. – effective against mycobacterium and strictly anaerobic bacteria, and against the spores and fungi of the Candida species

ANTI-PLAQUE AGENTS • Triclosan: – The mechanism of its antiseptic action is by acting on the microbial cytoplasmic membrane, inducing leakage of cellular constituents and thereby causing lysis of the micro-organisms.

ANTI-PLAQUE AGENTS • Triclosan: – Evidence has accumulated to suggest that triclosan in itself does not produce optimal plaque inhibitory effects without the addition of other chemicals which increase its antibacterial effect. • Most commonly used are copolymer PVM/MA and zinc citrate. They enhance surface retention of triclosan

ANTI-PLAQUE AGENTS • Triclosan: – Triclosan also has antiinflammatory effect by acting on the eicosanoid-cascade. – Triclosan inhibits both cyclooxygenase (COX) and lipoxygenase (LOX), and thereby inhibits the production of prostaglandins and leukotrienes – Clinical studies also indicate that triclosan reduces oral mucosal irritation caused by sodium lauryl sulphate (SLS)

ANTI-PLAQUE AGENTS • Metal-ions: – zinc (Zn2+) and stannous (Sn2+) • most widely used metal-ions in dental preparations – – – – These metals have the ability to limit bacterial growth, inhibit plaque formation, inhibit the glycolytic sequence in oral anaerobic bacteria, – restrict the ability of plaque bacteria to convert urea to ammonia

ANTI-PLAQUE AGENTS • Stannous- ions: – Stannous-ions are added to dentifrices and mouthwashes in the form of stannous fluoride or stannous pyrophosphate. – Stannous fluoride was frequently used as a vehicle for fluoride in dental preparations in the 1960s and 1970s. – At present time it is rarely used

ANTI-PLAQUE AGENTS • Stannous- ions: – Mouth rinses containing stannous fluoride have been found to reduce the relative amounts of S. Mutans and S. Sanguis in plaque, to reduce the population of S. Mutans in saliva and to increase the salivary levels of lactobacilli

ANTI-PLAQUE AGENTS • Stannous- ions: – The stannous fluoride treated enamel becomes hydrophobic, a property which may contribute to the antiplaque effect of stannous fluoride, since hydrophobic surfaces are less easily colonised by bacteria – The cariostatic protection provided by stannous fluoride is dependent on a deposition of CaF reservoir on the tooth surface (Fluoride theory nr 3)

ANTI-PLAQUE AGENTS • Stannous- ions: – Both the antiplaque effect and the inhibition of acid formation by stannous fluoride are most likely caused by the oxidation of thiol groups which stannous fluoride is known to perform. – Stannous ions may inhibit bacterial glycolysis because the enzymes depend on the thiol group for their biological activity . – The antiplaque effect of SnF can clearly also contribute to the cariostatic activity.

ANTI-PLAQUE AGENTS • Zinc ions: – Zinc is added to toothpastes and mouthwashes as zinc chloride or zinc citrate. – Zinc is a relatively non-toxic, non-cumulative essential trace element – Zinc inhibits the PTS pathway of glucose uptake by S. Mutans, S. Sanguis and Actinomyses naeslundii, and the metabolism of glucose to lactic acid.

ANTI-PLAQUE AGENTS • Essential oils: – Essentials oils of thymol, menthol, eucalyptol and methyl salicylate are thought to have anti-bacterial activity by altering the bacterial cell wall. – Mouth rinses containing these active ingredients have been reported to reduce plaque and gingivitis significantly.

ANTI-PLAQUE AGENTS • Chlorhexidine: – Chlorhexidine formulations are considered to be the “gold standard” antiplaque mouthrinses due to their prolonged broad activity and plaque inhibitory potential

ANTI-PLAQUE AGENTS • Chlorhexidine: – Chlorhexidine is effective against both Grampositive and Gram-negative bacteria, but has most effect against Gram-positive bacteria. – Chlorhexidine is bacteriostatic at very low concentrations, especially against S. mutans. – It also has effect against fungi,. And some viruses but non or little effect against spores

ANTI-PLAQUE AGENTS • Chlorhexidine: – Chlorhexidine is retained in the oral cavity for 24 hours by binding to phosphate, sulphate and carboxyl groups in bacteria, plaque, saliva and on the enamel surface. – The anti-bacterial action is due to a disturbance of the transport through the cell membrane and of the bacterial metabolism, and by causing leakage through the cell membrane.

ANTI-PLAQUE AGENTS • Chlorhexidine: – Its antiviral effect is caused by interaction with the viral protein cap. – It is also reported that chlorhexidine affects the chemotaxis, release of free oxygen radicals and degranulation by the polymorph nuclear neutrophile leucocytes, and thereby has an influence on the inflammatory process

ANTI-PLAQUE AGENTS • Chlorhexidine: – Sodium lauryl sulphate appears to adversely affect the retention of chlorhexidine and its plaqueinhibiting action. Rinsing with chlorhexidine should therefore not be performed in combination with tooth brushing. – Sodium monofluoride, stannous fluoride and Nystatin also dramatically reduces the effect of chlorhexidine

ANTI-CALCULUS AGENTS • Pyrophosphate – Pyrophosphate has recently been introduced in dentifrices to inhibit the formation of supragingival dental calculus. – Pyrophosphate is added as tetrasodium pyrophosphate, tetrapotassium pyrophosphate or disodium pyrophosphate.

ANTI-CALCULUS AGENTS • Pyrophosphate – It has been shown that pyrophosphate has high affinity to hydroxyapatite (HA) surfaces, probably by an interaction with Ca2+in the hydration layer. By interacting with HA and the enamel surface, pyrophosphate reduces their protein-binding capacity. – It also has the ability to inhibit calcium phosphate formation. It is therefore conceivable that pyrophosphate introduced in the oral cavity through dentifrices may affect pellicle formation.

ANTI-CALCULUS AGENTS • Pyrophosphate – The tartar control dentifrices that contain pyrophosphate as a calculus inhibitor also incorporate phosphates inhibitors that prolong the activity of pyrophosphate in the mouth. – Studies have indicated that fluoride in combination with PVM/MA Copolymer gives a significant protection of pyrophosphate against phosphatases

ANTI-DENTINE HYPERSENSITIVITY AGENTS • Potassium salts – Potassium ions are thought to act by blocking action potential generation in intradental nerves – It is claimed that potassium salts in dental preparations increase the concentration of potassium ions around the pulpal nerves, and thereby depolarises the nerve. This can inhibit a nerve response from different stimuli

WHITENING AGENTS • Abrasives: – An abrasive is required for the effective removal of a discoloured pellicle. – Abrasives provide a significant whitening benefit, particularly on smooth surfaces, but are of limited use for areas along the gum line and interproximally – Some whitening toothpastes contain coarse abrasives that can damage the dental tissue

WHITENING AGENTS • Dimethicones: – Dimethicones are versatile substances that ranges from low molecular weight polydimethylsioxane fluids to high molecular weight polymers that are gum-like in nature – They cause a smooth surface on the tooth that prevents stain formation.

WHITENING AGENTS • Papain: – Papain is a sulfhydryl protease consisting of a single polypeptide chain, extracted from the Carica papayaplant. – It is able to hydrolyse peptid bonds, and can also catalyse the transfer of an acyl group. It is used in toothpastesas an non-abrasive whitening

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